METHOD FOR THE MANUFACTURE OF DEGARELIX

METHOD FOR THE MANUFACTURE OF DEGARELIX

In a step-wise synthesis of degarelix comprising 0.3% by weight or less of 4-([2-(5-hydantoyl)]acetylamino)-phenylalanine analog on (solid support)-NH2 a step comprises providing a solution of an amino acid or peptide of which the α-amino group is protected by Fmoc; contacting the support with the s...

Ausführliche Beschreibung

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Bibliographische Detailangaben
Hauptverfasser: FOMSGAARD, Jens, ZHANG, Haixiang, STAERKAER, Gunnar
Format: Patent
Sprache:eng ; hun
Schlagworte:
CHEMISTRY
METALLURGY
ORGANIC CHEMISTRY
PEPTIDES
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Beschreibung
Zusammenfassung:In a step-wise synthesis of degarelix comprising 0.3% by weight or less of 4-([2-(5-hydantoyl)]acetylamino)-phenylalanine analog on (solid support)-NH2 a step comprises providing a solution of an amino acid or peptide of which the α-amino group is protected by Fmoc; contacting the support with the solution in the presence of reagent for forming a peptide bond between a carboxyl group of the amino acid or peptide and (solid support)-NH2; removing Fmoc by contacting the support with an organic base, in particular piperidine, in an organic solvent. Also disclosed is degarelix of high purity prepared by the method of the invention and the use of Fmoc in the synthesis of degarelix.